JP5579197B2 - インドロカルバゾール化合物のポリマー結合体の合成 - Google Patents

インドロカルバゾール化合物のポリマー結合体の合成 Download PDF

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JP5579197B2
JP5579197B2 JP2011542820A JP2011542820A JP5579197B2 JP 5579197 B2 JP5579197 B2 JP 5579197B2 JP 2011542820 A JP2011542820 A JP 2011542820A JP 2011542820 A JP2011542820 A JP 2011542820A JP 5579197 B2 JP5579197 B2 JP 5579197B2
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unsubstituted
polymer
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unsubstituted lower
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JP2012513447A (ja
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バニョード ラファエッラ
ベッカリア ルカ
ベルタリオーネ ラヴァ ロッサ ルイーザ
クリスクオーロ ドメニコ
ロレンツェット キアラ
マイネーロ ヴァレンティナ
マルコーニ アレッサンドラ
ピンチェリ カルロ
トラヴェルザ シルヴィオ
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CREABILIS SA
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/80—[b, c]- or [b, d]-condensed
    • C07D209/82—Carbazoles; Hydrogenated carbazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P3/00—Drugs for disorders of the metabolism
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/24—Oxygen atoms
    • C07D243/30—Preparation including building-up the benzodiazepine skeleton from compounds already containing hetero rings
    • C07D243/36—Preparation including building-up the benzodiazepine skeleton from compounds already containing hetero rings containing an indole or hydrogenated indole ring system

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Communicable Diseases (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Transplantation (AREA)
  • Psychiatry (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Reproductive Health (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP2011542820A 2008-12-22 2009-12-22 インドロカルバゾール化合物のポリマー結合体の合成 Active JP5579197B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US13981608P 2008-12-22 2008-12-22
US61/139,816 2008-12-22
US15205509P 2009-02-12 2009-02-12
US61/152,055 2009-02-12
PCT/EP2009/067817 WO2010072795A1 (fr) 2008-12-22 2009-12-22 Synthèse de conjugués polymères de composés de l'indolocarbazole

Publications (2)

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JP2012513447A JP2012513447A (ja) 2012-06-14
JP5579197B2 true JP5579197B2 (ja) 2014-08-27

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JP2011542820A Active JP5579197B2 (ja) 2008-12-22 2009-12-22 インドロカルバゾール化合物のポリマー結合体の合成

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US (1) US8926955B2 (fr)
EP (1) EP2381964B1 (fr)
JP (1) JP5579197B2 (fr)
KR (1) KR101431165B1 (fr)
CN (1) CN102264398B (fr)
AU (1) AU2009331490C1 (fr)
BR (1) BRPI0923583A2 (fr)
CA (1) CA2747838C (fr)
CY (1) CY1115529T1 (fr)
DK (1) DK2381964T3 (fr)
ES (1) ES2484000T3 (fr)
HK (1) HK1162978A1 (fr)
HR (1) HRP20140836T1 (fr)
IL (1) IL213516A (fr)
MX (1) MX2011006456A (fr)
MY (1) MY171292A (fr)
NZ (1) NZ593438A (fr)
PL (1) PL2381964T3 (fr)
PT (1) PT2381964E (fr)
RS (1) RS53530B1 (fr)
RU (1) RU2532341C2 (fr)
SG (1) SG172346A1 (fr)
SI (1) SI2381964T1 (fr)
SM (1) SMT201400141B (fr)
WO (1) WO2010072795A1 (fr)
ZA (1) ZA201104289B (fr)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014177510A2 (fr) * 2013-05-03 2014-11-06 Creabilis Sa Conjugués polymères de composés indolocarbazole dans le traitement du prurit
JP6445802B2 (ja) * 2014-07-16 2018-12-26 学校法人慶應義塾 インフラマソーム活性化制御物質のスクリーニング方法
EP3600440A1 (fr) 2017-03-20 2020-02-05 Sienna Biopharmaceuticals, Inc. Conjugués d'exposition réduite modulant des cibles thérapeutiques
WO2018175302A1 (fr) 2017-03-20 2018-09-27 Sienna Biopharmaceuticals, Inc. Conjugués polymères ciblant c-src à exposition réduite
WO2018175315A1 (fr) 2017-03-20 2018-09-27 Sienna Biopharmaceuticals, Inc. Conjugués polymères-dérivés de staurosporine permettant une exposition réduite
WO2018175301A1 (fr) 2017-03-20 2018-09-27 Sienna Biopharmaceuticals, Inc. Conjugué polymère-motesanib à exposition réduite
EP3621657A1 (fr) 2017-05-10 2020-03-18 Sienna Biopharmaceuticals, Inc. Utilisations de conjugués polymères de composés indolocarbazole à exposition réduite
US20190209472A1 (en) * 2017-12-04 2019-07-11 Sienna Biopharmaceuticals, Inc. Formulations for dermal delivery of polymer conjugates of indolocarbazole compounds with reduced exposure
WO2020023387A1 (fr) * 2018-07-23 2020-01-30 Sienna Biopharmaceuticals, Inc. Utilisations de conjugués polymères de composés indolocarbazole à exposition réduite

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5013556A (en) 1989-10-20 1991-05-07 Liposome Technology, Inc. Liposomes with enhanced circulation time
WO1993024476A1 (fr) 1992-06-04 1993-12-09 Clover Consolidated, Limited Vehicules polymeres solubles dans l'eau servant a la liberation de medicaments
US6326353B1 (en) * 1993-03-23 2001-12-04 Sequus Pharmaceuticals, Inc. Enhanced circulation effector composition and method
US5468872A (en) 1993-09-16 1995-11-21 Cephalon, Inc. K-252a functional derivatives potentiate neurotrophin-3 for the treatment of neurological disorders
UA67725C2 (en) * 1996-06-03 2004-07-15 Cephalon Inc K-252a derivatives and a method for improvement of functioning and cell survival enhancement
US20060210553A1 (en) 2003-07-23 2006-09-21 Creabilis Therapeutics S.R.L. Topical use of tyrosine kinase inhibitors of microbial origin to prevent and treat skin disorders characterised by excesssive cell proliferation
ES2306195T3 (es) 2004-07-02 2008-11-01 Creabilis Therapeutics S.P.A. Agentes terapeuticos para el tratamiento de patologias relacionas con hmgb1.
NZ566160A (en) 2005-08-25 2010-12-24 Creabilis Therapeutics Spa Polymer conjugates of K-252A and derivatives thereof

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Publication number Publication date
US20110311451A1 (en) 2011-12-22
CA2747838A1 (fr) 2010-07-01
RU2532341C2 (ru) 2014-11-10
CN102264398B (zh) 2013-12-18
SMT201400141B (it) 2014-11-10
CN102264398A (zh) 2011-11-30
HRP20140836T1 (hr) 2014-10-10
AU2009331490C1 (en) 2013-11-28
AU2009331490A1 (en) 2011-07-14
WO2010072795A1 (fr) 2010-07-01
MY171292A (en) 2019-10-07
SG172346A1 (en) 2011-07-28
PT2381964E (pt) 2014-08-29
RS53530B1 (en) 2015-02-27
ZA201104289B (en) 2012-02-29
DK2381964T3 (da) 2014-09-29
KR20110118630A (ko) 2011-10-31
MX2011006456A (es) 2011-10-11
IL213516A0 (en) 2011-07-31
PL2381964T3 (pl) 2014-11-28
US8926955B2 (en) 2015-01-06
ES2484000T3 (es) 2014-08-08
NZ593438A (en) 2012-12-21
EP2381964A1 (fr) 2011-11-02
SI2381964T1 (sl) 2014-10-30
JP2012513447A (ja) 2012-06-14
HK1162978A1 (en) 2012-09-07
BRPI0923583A2 (pt) 2018-10-09
CA2747838C (fr) 2013-07-02
IL213516A (en) 2015-02-26
KR101431165B1 (ko) 2014-08-18
CY1115529T1 (el) 2017-01-04
EP2381964B1 (fr) 2014-06-25
RU2011130512A (ru) 2013-01-27
AU2009331490B2 (en) 2013-08-22

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